Microwave Assisted Synthesis and Pharmacological Evaluation of Few 4-Quinazolinone Derivatives
By: Rishipathak, Dinesh D
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Contributor(s): Jadhav, Trupti A.
Description: 147-154p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Asian journal of pharmaceutical researchSummary: In the present investigation, 3-(4-oxo-2-phenyiquinazolin-3(4H)-yl)-2-(substituted phenyl) thiazolidin -4-one derivatives were synthesized with the aim of achieving compounds with anticonvulsant potential. The docking study was performed by 1KJT receptor and yielded good score. The microwave assisted heating technique used which is rapid and efficient resulting in reduced reaction times and increased yields compared to conventional technique. The synthesized compounds were confirmed on the basis of IR, 1H-NMR and Mass analyses. Some of the synthesized compounds were evaluated for their anticonvulsant effect by PTZ induced convulsions method. The molecular docking studies resulted in highlighting the ligands and their conformations which efficiently fit into the cavity #1 of target protein GABA (A)- receptor- associated protein (1KJT). The pharmacological evaluation of the compounds showed increase in latency (onset time) to induce convulsions; decrease in the number of convulsions and increase in latency of death compared to control. From the series of 3-(4-oxo-2-phenylquinazolin-3(4H)-yl)-2-(substitutedphenyl)-thiazolidin-4-ones; compounds viz. AQCI-C2, AQPC-C4, AQBE-C5, AQFU-C6 fitted best into the cavity of 1KJT with lowest dock score. The compound AQBE-9 shows highest latency as 4.16 minutes at the dose of 270mg/kg. The compounds AQCI-4and AQBE-9 showed highest percentage of protection (80%) at the dose of 270 mg/kg among the evaluated compounds compared to control. The analysis of structural features revealed that substitution of cinnamyl group and phenyl group on Thiazolidinone ring showed enhanced the anticonvulsant potential among the synthesized compounds.
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School of Pharmacy Archieval Section | Not for loan | 2020668 |
In the present investigation, 3-(4-oxo-2-phenyiquinazolin-3(4H)-yl)-2-(substituted phenyl) thiazolidin -4-one derivatives were synthesized with the aim of achieving compounds with anticonvulsant potential. The docking study was performed by 1KJT receptor and yielded good score. The microwave assisted heating technique used which is rapid and efficient resulting in reduced reaction times and increased yields compared to conventional technique. The synthesized compounds were confirmed on the basis of IR, 1H-NMR and Mass analyses. Some of the synthesized compounds were evaluated for their anticonvulsant effect by PTZ induced convulsions method. The molecular docking studies resulted in highlighting the ligands and their conformations which efficiently fit into the cavity #1 of target protein GABA (A)- receptor- associated protein (1KJT). The pharmacological evaluation of the compounds showed increase in latency (onset time) to induce convulsions; decrease in the number of convulsions and increase in latency of death compared to control. From the series of 3-(4-oxo-2-phenylquinazolin-3(4H)-yl)-2-(substitutedphenyl)-thiazolidin-4-ones; compounds viz. AQCI-C2, AQPC-C4, AQBE-C5, AQFU-C6 fitted best into the cavity of 1KJT with lowest dock score. The compound AQBE-9 shows highest latency as 4.16 minutes at the dose of 270mg/kg. The compounds AQCI-4and AQBE-9 showed highest percentage of protection (80%) at the dose of 270 mg/kg among the evaluated compounds compared to control. The analysis of structural features revealed that substitution of cinnamyl group and phenyl group on Thiazolidinone ring showed enhanced the anticonvulsant potential among the synthesized compounds.
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